Patent SG-11201903908P-A (SG)
Title: Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
Inventor: BOUABOULA MONSIF
IPC: C07D411/12
Filed: 2017-07-21
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111 IOU 0 11101 010 11111 OIE 10001101111113 OIE 1011 00 111110 HOED Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/091153 Al 24 May 2018 (24.05.2018) WIP0 1 PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every CO7D 403/12 (2006.01) CO7D 411/12 (2006.01) kind of national protection available): AE, AG, AL, AM, CO7D 401/14 (2006.01) CO7D 471/04 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CO7D 405/14 (2006.01) CO7D 207/12 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, CO7D 413/14 (2006.01) A61K 31/4025 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, CO7D 401/12 (2006.01) A61P 35/00 (2006.01) HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, CO7D 405/12 (2006.01) A61P 37/00 (2006.01) KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, CO7D 409/12 (2006.01) A61P 5/32 (2006.01) MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, CO7D 409/14 (2006.01) A61P 19/10 (2006.01) OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (21) International Application Number: SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, PCT/EP2017/068446 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (22) International Filing Date: (84) Designated States (unless otherwise indicated, for every 21 July 2017 (21.07.2017) kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (25) Filing Language: English UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (26) Publication Language: English TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (30) Priority Data: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, 16306506.3 17 November 2016 (17.11.2016) EP TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). — (71) Applicant: SANOFI [FR/FR]; 54 me La Boetie, 75008 PARIS (FR). Declarations under Rule 4.17: = Inventors: BOUABOULA, Monsif; c/o Sanofi, Patent — of inventorship (Rule 4.17(iv)) (72) Department, Mail Stop: 55A-505A, 55 Corporate Drive, Published: Bridgewater, New Jersey 08807 (US). BROLLO, Mau- rice; c/o Sanofi, Patent Department, 54 rue La Boetie, 75008 — with international search report (Art. 21(3)) = _ PARIS (FR). CERTAL, Victor; c/o Sanofi, Patent De- = 54 me La Boetie, 75008 PARIS (FR). EL-AH- _ _ partment, MAD, Youssef; c/o Sanofi, Patent Department, 54 rue La Boetie, 75008 PARIS (FR). FILOCHE-ROMME, Bruno; c/o Sanofi, 54 rue La Boetie, 75008 PARIS (FR). HAL- — _ = LEY, Frank; c/o Sanofi, 54 me La Boetie, 75008 PARIS (FR). MCCORT, Gary; c/o Sanofi, 54 rue La Boetie, 75008 PARIS (FR). SCHIO, Laurent; c/o Sanofi, 54 rue = = La Boetie, 75008 PARIS (FR). TABART, Michel; c/o Sanofi, 54 me La Boetie, 75008 PARIS (FR). TERRIER, Corinne; c/o Sanofi, 54 me La Boetie, 75008 PARIS (FR). = _ THOMPSON, Fabienne; c/o Sanofi, 54 rue La Boetie, 75008 PARIS (FR). = = = Agent: ROMANOWSKI, Caroline; c/o Sanofi, Patent De- (74) = partment, 54 rue La Boetie, 75008 PARIS (FR). = Title: NOVEL SUBSTITUTED N-(3-FLUOROPROPYL)-PYRROLIDINE COMPOUNDS, PROCESSES FOR THEIR — (54) - PREPARATION AND THERAPEUTIC USES THEREOF (57) : The present invention relates to novel substituted N-(3-fluoro- en in propy1)-pyrrolidine compounds of formula (1-A): wherein R1 and R2 represent indepen- R2 R1 1-1 dently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; 1-1 N and SERM-F represents a selective estrogen receptor modulator fragment comprising an 01 0 --.... aryl or heteroaryl group linked to the adjacent \"A\" group. The invention also relates to the A preparation and to the therapeutic uses of the compounds of formula (1-A) as inhibitors 1-1 / and degraders of estrogen receptors. cz ei SERM-F (I-A) O